IDH2 mutation-induced histone and DNA hypermethylation is progressively reversed by small-molecule inhibition.

@article{Kernytsky2015IDH2MH,
  title={IDH2 mutation-induced histone and DNA hypermethylation is progressively reversed by small-molecule inhibition.},
  author={Andrew Kernytsky and Fang Wang and Erica B. Hansen and Stefanie S. Schalm and Kimberly S. Straley and Camelia Gliser and Hua Yang and Jeremy M. Travins and Stuart Murray and Marion Dorsch and Sam Agresta and David P. Schenkein and Scott A. Biller and Shinsan M. Su and Wei Liu and Katharine E. Yen},
  journal={Blood},
  year={2015},
  volume={125 2},
  pages={
          296-303
        }
}
Mutations of IDH1 and IDH2, which produce the oncometabolite 2-hydroxyglutarate (2HG), have been identified in several tumors, including acute myeloid leukemia. Recent studies have shown that expression of the IDH mutant enzymes results in high levels of 2HG and a block in cellular differentiation that can be reversed with IDH mutant-specific small-molecule inhibitors. To further understand the role of IDH mutations in cancer, we conducted mechanistic studies in the TF-1 IDH2 R140Q… CONTINUE READING

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